Novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA.

Novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA. Research Abstract Details 

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Novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA. Abstract Text:

Jianhui Wu,Guohui Cui,Ming Zhao,Chunying Cui,Shiqi Peng,Jianhui Wu,Guohui Cui,Ming Zhao,Chunying Cui,Shiqi Peng,Jianhui Wu,Guohui Cui,Ming Zhao,Chunying Cui,Shiqi Peng,

To explore the intercalating mechanism of beta-carbolines, four novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids [-phenylalanine (), -alanine (), -isoleucine () and -glycine ()] were prepared here. Their in vitro anticancer activities were examined by their anti-proliferation for 5 human carcinoma cell lines. The average IC(50)s against 5 human carcinoma cell lines are 53.54 microM, 118.77 microM, 147.34 microM and greater than 291.63 microM for , , and , respectively. The DNA intercalating mechanism of was approved by the comparison of the parameters and signals of UV, CD and fluorescence spectra of calf thymus DNA (CT DNA) alone and the CT DNA/ system. Using fluorescence titration based kinetic analysis a two-step-course consisting of stacking and intercalating was described and the stacking was considered as the key step to the CT DNA intercalating mechanism of . Using fluorescence titration based thermomechanical analysis, the stacking complexes of with CT DNA were described to be formed spontaneously and to be stabilized predominantly by their hydrophobic interactions. The intercalation itself goes very fast and only has limited contribution to their anticancer activities.

Novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA. Publishing Authors By Initials

J Wu,G Cui,M Zhao,C Cui,S Peng,J Wu,G Cui,M Zhao,C Cui,S Peng,J Wu,G Cui,M Zhao,C Cui,S Peng,

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Novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Molecular bioSystems

VOLUME: 3

Page Numbers: 855-61

Journal Abbreviation: Mol Biosyst

ISSN: 1742-206X

DAY: 2

MONTH: 10

YEAR: 2007

Novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA. Information

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LANGUAGE: eng

NlmUniqueID: 101251620

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Grant and Affiliation Information for Novel N-(3-carboxyl-9-benzylcarboline-1-yl)ethylamino acids: synthesis, anti-proliferation activity and two-step-course of intercalation with calf thymus DNA.

AFFILIATION: College of Pharmaceutical Sciences, Peking University, Beijing 100083, P. R. China.

Country: England

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MEDLINETA: Mol Biosyst

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